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Creation and Use of 12-LO inhibitors (4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives) for the Treatment of Diabetes and Large Platelet-Derived Clots

This technology includes the discovery and use of novel selective 12-LO (lipoxygenase) inhibitors, 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives, for attenuating large clots and for the treatment of Type 1/2 diabetes. A 12-LO inhibitor could be a potent intracellular approach to block platelets from forming large clots in response...

Published: 7/25/2024 | Inventor(s): Ajit Jadhav, Anton Simeonov, Adam Yasgar, Diane Luci, Michael Holinstat, Theodore Holman, Jerry Nadler, David Taylor-Fishwick, David Maloney

Keywords(s): 12-Lipoxygenase., 4-2-hydroxy-3-methoxybenzylaminobenzenesulfon, Derivatives, Discovery, Human, Inhibitors, Listed LPM Nguyen-Antczak as of 4/15/2015, Post LPM Assignment Set 20150420, POTENT, Pre LPM working set 20150418, SELECTIVE, VDXXXX, VFXXXX, WKXXXX, XEXXXX

Category(s): TherapeuticArea > Cardiology, TherapeuticArea > Endocrinology, Application > Therapeutics

Potent Nucleotide Inhibitors of Ecto-5'-Nucleotidase (CD73)

These small molecules are novel nucleotide derivatives, containing either a purine or pyrimidine nucleobase, that competitively block the enzyme CD73, also known as ecto-5'-nucleotidase. This enzyme converts extracellular AMP (not a potent activator of adenosine receptors) to adenosine (the native activator of 4 subtypes of adenosine receptors. CD73...

Published: 7/25/2024 | Inventor(s): Christa Mueller, Anna Junker, Kenneth Jacobson

Keywords(s): CB5EXX, CD73, Ecto-5-nucleotidase, Inhibitors, Nucleotide, POTENT

Category(s): Collaboration Sought > Collaboration, TherapeuticArea > Oncology, Application > Therapeutics

N6, A Novel, Broad, Highly Potent HIV-specific Antibody

This is a new antibody coming out of NIAID’s intramural program. N6 has evolved a unique mode of binding that depends less on a variable area of the HIV envelope known as the V5 region and focuses more on conserved regions, which change relatively little among HIV strains. This allows N6 to tolerate changes in the HIV envelope, including the attachment...

Published: 7/25/2024 | Inventor(s): Jinghe Huang, Byong Kang, John Mascola, Elise Ishida, Tongqing Zhou, Anqi Zheng, Peter Kwong, Mark Connors

Keywords(s): ANTIBODY, bNAb, Broad, Highly, HIV-soecific, HIV-Specific, Listed LPM Thalhammer-Reyero as of 4/15/2015, N6, Novel, Ootent, Post LPM Assignment Set 20150420, POTENT, Pre LPM working set 20150418

Category(s): Collaboration Sought > Collaboration

Highly Potent and Selective Deubiquitinating Enzyme Inhibitor

Available for licensing are inhibitors that target the USP1/ UAF1 deubiquitinating enzyme (DUB) complex. The FDA approval and commercial success of Velcade®, a small molecule proteasome inhibitor, has established the ubiquitin-proteasome system (UPS) as a valid target for anticancer treatment. However, proteasome inhibitors in general suffer from...

Published: 7/29/2024 | Inventor(s): Andrew Rosenthal, Ajit Jadhav, Thomas Dexheimer, Anton Simeonov, Qin Liang, Zhihao Zhuang, David Maloney

Keywords(s): CANCER, CANCER THERAPEUTICS, CB5XXX, CB7XXX, CBXXXX, Combination Therapy, CXXXXX, Deubiquitinase, Inhibitors, POTENT, protease inhibitors, SELECTIVE, small molecule, USP1/UAF1

Category(s): Collaboration Sought > Collaboration, Collaboration Sought > Licensing, TherapeuticArea > Oncology, Application > Therapeutics

Small Molecule MRS5474 with Anticonvulsant Activity for Treatment of Epilepsy

Adenosine modulates many physiological processes by activating specific adenosine receptors. These adenosine receptors play a critical role in the regulation of cellular signaling and are broadly distributed throughout the body. Thus, the ability to modulate adenosine receptor-mediated signaling is an attractive therapeutic strategy for a broad range...

Published: 7/25/2024 | Inventor(s): Dilip Tosh, Kenneth Jacobson

Keywords(s): A3, Activity, ADENOSINE, AGONISTS, Agonists:, Al, ANTAGONISTS, Anticonvulsant, Derivatives, Docking, IB1FXX, IB1XXX, IBXXXX, IXXXXX, NB1EXX, NB1HXX, NB1XXX, NBXXXX, N-Methanocarba, Nucleosides, NXXXXX, PARTIAL, Patent Category - Chemistry, POTENT, RECEPTOR, TRUNCATED

Category(s): Collaboration Sought > Collaboration, TherapeuticArea > Neurology, Application > Diagnostics, Application > Research Materials, TherapeuticArea > Cardiology, Application > Therapeutics

Novel Small Molecule Agonists of the Relaxin Receptor as Potential Therapy for Heart Failure and Fibrosis

The present invention is directed to novel small molecule agonists of the mammalian relaxin family receptor 1 (RXFP1), including human RXFP1. Activation of RXFP1 induces: 1) vasodilation due to up-regulation of the endothelin system; 2) extracellular matrix remodeling; 3) moderation of inflammation by reducing levels of inflammatory cytokines; and...

Published: 7/25/2024 | Inventor(s): Wei Zheng, Marc Ferrer-Alegre, Catherine Chen, Alexander Agoulnik, Noel Southall, Jingbo Xiao, Juan Marugan

Keywords(s): 1, IB1XXX, IB3XXX, IB5XXX, IB6XXX, IBXXXX, IXXXXX, MODULATORS, POTENT, RECEPTOR, Relaxin, RXFP1, SELECTIVE

Category(s): Collaboration Sought > Collaboration, Application > Therapeutics, Application > Vaccines, TherapeuticArea > Cardiology, TherapeuticArea > Reproductive Health, TherapeuticArea > Immunology, Application > Research Materials, Application > Diagnostics

Potent and Selective Cyclic Peptide Inhibitors of Phosphoglycerate Mutase as Anti-Infective Agents

Summary – The invention includes compounds and compositions for inhibiting phosphoglycerate mutase (PGM) activity. In some examples, the compounds selectively inhibit cofactor-independent PGM (iPGM). In particular embodiments, the compounds include one or more cyclic peptides. Brief Background – Co-factor independent phosphoglycerate mutase (iPGM)...

Published: 7/25/2024 | Inventor(s): Patricia Dranchak, Ryan Macarthur, James Inglese

Keywords(s): Agents, Anti-infective, Cyclic, DB2XXX, DB3XXX, Inhibitors, Mutase, Peptide, Phosphoglycerate, POTENT, SELECTIVE, VJXXXX, VQXXXX

Category(s): Collaboration Sought > Collaboration, Collaboration Sought > Licensing, TherapeuticArea > Infectious Disease, Application > Therapeutics